Research Topics
| D M VigushinSummaryAffiliation: Imperial College Country: UK Publications
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Publications
Histone deacetylase inhibitor, trichostatin A induces ubiquitin-dependent cyclin D1 degradation in MCF-7 breast cancer cellsJohn P Alao
Department of Cancer Medicine, Imperial College, Hammersmith Hospital, London, W12 0NN, UK
Mol Cancer 5:8. 2006..TSA treatment also resulted in accumulation of polyubiquitylated GFP-cyclin D1 species and reduced levels of the recombinant protein within the nucleus...
The cyclin D1 proto-oncogene is sequestered in the cytoplasm of mammalian cancer cell linesJohn P Alao
Department of Cancer Medicine, Imperial College, Hammersmith Hospital, London, W12 0NN, UK
Mol Cancer 5:7. 2006..Additional studies were initiated in order to further investigate the effect of TSA on cyclin D1 regulation using sub-cellular fractionation techniques...
The nuclear oxysterol receptor LXRalpha is expressed in the normal human breast and in breast cancerD M Vigushin
Department of Cancer Medicine, Imperial College London, Hammersmith Hospital Campus, Du Cane Road, London W12 0NN
Med Oncol 21:123-31. 2004..Inhibition of breast cancer cell proliferation suggests that pharmacological LXRalpha agonists may have potential preventive and/or therapeutic antitumor activity in breast cancer...
Pyrazino[1,2-a]indole-1,4-diones, simple analogues of gliotoxin, as selective inhibitors of geranylgeranyltransferase IDavid M Vigushin
Department of Cancer Medicine, 6th Floor MRC Cyclotron Building, Imperial College of Science, Technology and Medicine, Hammersmith Hospital Campus, Du Cane Road, London W12 0NN, UK
Bioorg Med Chem Lett 13:3661-3. 2003....
Gliotoxin is a dual inhibitor of farnesyltransferase and geranylgeranyltransferase I with antitumor activity against breast cancer in vivoD M Vigushin
Department of Cancer Medicine, 6th Floor MRC Cyclotron Building, Imperial College London, Hammersmith Hospital Campus, Du Cane Road, London W12 0NN, UK
Med Oncol 21:21-30. 2004..The present studies confirm that gliotoxin is a dual inhibitor of farnesyltransferase and geranylgeranyltransferase I with pronounced antitumor activity and favorable toxicity profile against breast cancer in vitro and in vivo...
Targeted histone deacetylase inhibition for cancer therapyD M Vigushin
Department of Cancer Medicine, Imperial College, Hammersmith Campus, London W12 0NN, UK
Curr Cancer Drug Targets 4:205-18. 2004..This report reviews the biology and clinical development of histone deacetylase inhibitors for cancer therapy...
Trichostatin A is a histone deacetylase inhibitor with potent antitumor activity against breast cancer in vivoD M Vigushin
Department of Cancer Medicine, Cancer Research Campaign Laboratories, Imperial College of Science, Technology, and Medicine, Hammersmith Hospital, London, United Kingdom
Clin Cancer Res 7:971-6. 2001....
Plasma pharmacokinetics and metabolism of the histone deacetylase inhibitor trichostatin a after intraperitoneal administration to miceL Sanderson
Department of Cancer Medicine, 6th Floor MRC Cyclotron Building, Imperial College London (Hammersmith Hospital Campus, Du Cane Road, London W12 0NN, United Kingdom
Drug Metab Dispos 32:1132-8. 2004..We conclude that trichostatin A is rapidly and extensively metabolized in vivo following intraperitoneal administration to mice, and N-demethylation does not compromise histone deacetylase-inhibitory activity...
Managing malignant disease in patients with porphyriaC Palmieri
Department of Cancer Medicine, Faculty of Medicine, Imperial College London, UK
QJM 97:115-26. 2004..We briefly review the biochemical basis, clinical features and current management of porphyria in cancer patients...
Structure-activity relationships of aryloxyalkanoic acid hydroxyamides as potent inhibitors of histone deacetylaseCharles M Marson
Department of Chemistry, University College London, Christopher Ingold Laboratories, 20 Gordon Street, London WC1H OAJ, UK
Bioorg Med Chem Lett 17:136-41. 2007..Variation of the substituents on the benzene ring as well as fusion of a second ring have marked effects on potency, in vitro IC(50) values down to 1 nM being obtained...
In vivo biological activity of the histone deacetylase inhibitor LAQ824 is detectable with 3'-deoxy-3'-[18F]fluorothymidine positron emission tomographyJulius Leyton
Molecular Therapy and Cancer Cell Biology, Imperial College London, Faculty of Medicine, Hammersmith Hospital, Du Cane Road, London W12 0NN, United Kingdom
Cancer Res 66:7621-9. 2006..Drug-induced changes in tumor [18F]FLT uptake were due, at least in part, to reductions in TK1 transcription and translation...
Histone deacetylase inhibitors in cancer treatmentDavid M Vigushin
Department of Cancer Medicine, Imperial College of Science, Technology and Medicine, Hammersmith Hospital Campus, London W12 0NN, UK
Anticancer Drugs 13:1-13. 2002..The focus of this review is the development and clinical application of HDAC inhibitors for the treatment of cancer...
Targeted histone deacetylase inhibition for cancer prevention and therapyCarlo Palmieri
Department of Cancer Medicine, 7th Floor MRC Cyclotron Building, Imperial College London, Hammersmith Hospital Campus, Du Cane Road, London W12 0NN, UK
Prog Drug Res 63:147-81. 2005
Histone deacetylase inhibitor trichostatin A represses estrogen receptor alpha-dependent transcription and promotes proteasomal degradation of cyclin D1 in human breast carcinoma cell linesJohn Patrick Alao
Department of Cancer Medicine, Imperial College London, Hammersmith Hospital Campus, Du Cane Road, London W12 0NN, United Kingdom
Clin Cancer Res 10:8094-104. 2004..Taken together, our data show that TSA effectively induces cyclin D1 down-regulation through both ERalpha-dependent and ERalpha-independent mechanisms, providing an important new strategy for combating resistance to antiestrogens...
ICI182,780 induces p21Waf1 gene transcription through releasing histone deacetylase 1 and estrogen receptor alpha from Sp1 sites to induce cell cycle arrest in MCF-7 breast cancer cell lineRana Varshochi
Cancer Research UK Laboratories and Section of Cancer Cell Biology, Department of Cancer Medicine, Imperial College London, Hammersmith Hospital Campus, Du Cane Road, London W12 ONN, United Kingdom
J Biol Chem 280:3185-96. 2005....
Increased gestational age at evacuation of a complete hydatidiform mole: does it correlate with increased risk of requiring chemotherapy?Michael J Seckl
Charing Cross Gestational Trophoblastic Disease Unit, Imperial College, London, UK
J Reprod Med 49:527-30. 2004..To assess whether a complete hydatidiform mole (CHM) carries an increased risk of later requiring chemotherapy in pregnancies continued to term...
FR-901228 Fujisawa/National Cancer InstituteDavid M Vigushin
Department of Cancer Medicine, MRC Cyclotron Building, Imperial College London, Hammersmith Hospital Campus, Du Cane Road, London W12 0NN, UK
Curr Opin Investig Drugs 3:1396-402. 2002..The depsipeptide FR-901228 is a histone deacetylas inhibitor under development by Fujisawa and the National Cancer Institute as a potential treatment for neoplasm. By May 2002, phase II trials had commenced in the US [452248], [461017]...
Stereodefined and polyunsaturated inhibitors of histone deacetylase based on (2E,4E)-5-arylpenta-2,4-dienoic acid hydroxyamidesCharles M Marson
Department of Chemistry, University College London, Christopher Ingold Laboratories, 20 Gordon Street, London WC1H OAJ, UK
Bioorg Med Chem Lett 14:2477-81. 2004..Variation of substituents on the aromatic ring has a marked effect on potency, in vitro IC(50) values down to 50 nM being obtained...
Quantification of cellular proliferation in tumor and normal tissues of patients with breast cancer by [18F]fluorothymidine-positron emission tomography imaging: evaluation of analytical methodsLaura M Kenny
Molecular Therapy and PET Oncology Research Group, Hammersmith Hospital, London, UK
Cancer Res 65:10104-12. 2005..We conclude that [18F]FLT-positron emission tomography is a promising clinical tool for imaging cellular proliferation in breast cancer, and is most predictive when analyzed by graphical and spectral methods...
Cyclic acid anhydrides as a new class of potent, selective and non-peptidic inhibitors of geranylgeranyl transferaseCharles M Marson
Department of Chemistry, University College London, Christopher Ingold Laboratories, 20 Gordon Street, London WC1H OAJ, UK
Bioorg Med Chem Lett 12:255-9. 2002..Cyclic acid anhydrides possessing a lipid chain have been shown to be a new class of non-peptidic inhibitors of geranylgeranyl protein-transferase type I (GGPTase-I)...
Imaging early changes in proliferation at 1 week post chemotherapy: a pilot study in breast cancer patients with 3'-deoxy-3'-[18F]fluorothymidine positron emission tomographyLaura Kenny
Imperial College London, and Hammersmith Hospital NHS Trust, London, UK
Eur J Nucl Med Mol Imaging 34:1339-47. 2007..The aims of this pilot study were to define objective criteria for [18F]FLT response and to examine whether [18F]FLT-PET can be used to quantify early response of breast cancer to chemotherapy...
